Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability
Dehydroepiandrosterone (DHEA) is an FDA-approved food supplement used as an assisted reproductive sex hormone. The bioavailability is severely limited by its poor solubility (23 µg/mL). Herein, we aimed to modulate its solubility through cocrystallization. Eight cocrystals of DHEA with pyrocatechol...
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MDPI AG
2022-11-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/11/2478 |
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| author | Yihua Jiang Yinxiang Cheng Mengyuan Xia Bingrui Zhang Qiaoce Ding Liye Lu Jian-Rong Wang Xuefeng Mei |
| author_facet | Yihua Jiang Yinxiang Cheng Mengyuan Xia Bingrui Zhang Qiaoce Ding Liye Lu Jian-Rong Wang Xuefeng Mei |
| author_sort | Yihua Jiang |
| collection | DOAJ |
| description | Dehydroepiandrosterone (DHEA) is an FDA-approved food supplement used as an assisted reproductive sex hormone. The bioavailability is severely limited by its poor solubility (23 µg/mL). Herein, we aimed to modulate its solubility through cocrystallization. Eight cocrystals of DHEA with pyrocatechol (CAT), hydroquinone (HQ), resorcinol (RES), phloroglucinol (PG), 1,5-dihydroxy naphthalene (DHN), p-hydroxybenzoic acid (PHBA), gallic acid (GA), and 5-hydroxyisophthalic acid (5HIPA) were designed and synthesized. Some basic characterization tools, including powder X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, and Fourier transform infrared spectroscopy, were also applied in our work for basic analyses of cocrystals. It is indicated that DHEA-GA exhibits its superiority in dissolution and pharmacokinetic behaviors. While the area under the curve values of DHEA-GA is improved at the ratio of 2.2, the corresponding bioavailability of DHEA is expected to be accordingly increased. |
| first_indexed | 2024-03-09T18:04:53Z |
| format | Article |
| id | doaj.art-ce6f126bf7ee4d30bd7c41bcae7ffa1c |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T18:04:53Z |
| publishDate | 2022-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-ce6f126bf7ee4d30bd7c41bcae7ffa1c2023-11-24T09:36:29ZengMDPI AGPharmaceutics1999-49232022-11-011411247810.3390/pharmaceutics14112478Dehydroepiandrosterone Cocrystals with Improved Solubility and BioavailabilityYihua Jiang0Yinxiang Cheng1Mengyuan Xia2Bingrui Zhang3Qiaoce Ding4Liye Lu5Jian-Rong Wang6Xuefeng Mei7Pharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaPharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaPharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaPharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaPharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaPharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaPharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaPharmaceutical Analytical & Solid-State Chemistry Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaDehydroepiandrosterone (DHEA) is an FDA-approved food supplement used as an assisted reproductive sex hormone. The bioavailability is severely limited by its poor solubility (23 µg/mL). Herein, we aimed to modulate its solubility through cocrystallization. Eight cocrystals of DHEA with pyrocatechol (CAT), hydroquinone (HQ), resorcinol (RES), phloroglucinol (PG), 1,5-dihydroxy naphthalene (DHN), p-hydroxybenzoic acid (PHBA), gallic acid (GA), and 5-hydroxyisophthalic acid (5HIPA) were designed and synthesized. Some basic characterization tools, including powder X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, and Fourier transform infrared spectroscopy, were also applied in our work for basic analyses of cocrystals. It is indicated that DHEA-GA exhibits its superiority in dissolution and pharmacokinetic behaviors. While the area under the curve values of DHEA-GA is improved at the ratio of 2.2, the corresponding bioavailability of DHEA is expected to be accordingly increased.https://www.mdpi.com/1999-4923/14/11/2478DHEAcocrystallizationcrystal structuresolubilitybioavailability |
| spellingShingle | Yihua Jiang Yinxiang Cheng Mengyuan Xia Bingrui Zhang Qiaoce Ding Liye Lu Jian-Rong Wang Xuefeng Mei Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability Pharmaceutics DHEA cocrystallization crystal structure solubility bioavailability |
| title | Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
| title_full | Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
| title_fullStr | Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
| title_full_unstemmed | Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
| title_short | Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
| title_sort | dehydroepiandrosterone cocrystals with improved solubility and bioavailability |
| topic | DHEA cocrystallization crystal structure solubility bioavailability |
| url | https://www.mdpi.com/1999-4923/14/11/2478 |
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